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1.发明授权Methods of inhibiting the ghrelin/growth hormone secretatogue receptor pathway and uses thereof 有权抑制生长素释放肽/生长激素分泌受体途径及其用途的方法公开(公告)号：US08883721B2
公开(公告)日：2014-11-11
申请号：US13320408
申请日：2010-05-12
IPC分类号： A61K38/08 , A61K38/10 , C07K7/06 , C07K7/08 , A61K31/00 , A61K45/06 , A61K31/404 , A61K38/16 , A61K38/25
CPC分类号： A61K38/08 , A61K31/00 , A61K31/404 , A61K38/10 , A61K38/16 , A61K38/25 , A61K45/06 , A61K2300/00
摘要： The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18 (SEQ ID NO: 93), wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.
摘要翻译： 本发明通过向受试者施用生长素释放肽O-酰基转移酶（GOAT）抑制剂和/或生长素释放肽受体拮抗剂来提供治疗，预防或控制受试者中肥胖症，肥胖相关病症，糖尿病和代谢综合征的方法。 本发明还提供式（VII）的生长素释放肽受体拮抗剂：A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18（SEQ ID NO：93），其中A11，A12 ，并且A13独立地不存在，氨基酸或氨基保护基; A15，A16，A17和A18各自独立地不存在或氨基酸; 并且A14是与-C（O）C1-C20烷基共轭的 - （O）C1-C20烷基或二氨基丙酸缀合的丝氨酸，条件是存在A11，A12或A13中的至少一种。
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2.发明授权Ghrelin/growth hormone releasing peptide/growth hormone secretatogue receptor antagonists and uses thereof 有权生长激素释放肽/生长激素释放肽/生长激素分泌受体拮抗剂及其用途公开(公告)号：US08536120B2
公开(公告)日：2013-09-17
申请号：US12298826
申请日：2007-04-30
IPC分类号： A61K31/15 , A61K31/216 , A61K38/08 , C07K7/06
CPC分类号： C07C233/75 , A61K38/00 , C07K7/02 , C07K7/06 , C07K14/60
摘要： The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，其形式和变体）的调节剂的新化合物。 这些化合物可用作生长素释放肽受体的拮抗剂以及反向激动剂，部分激动剂或这些活性的组合，作为治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病， 胃肠道疾病，心血管疾病，肥胖和肥胖相关疾病，糖尿病，中枢神经系统疾病，遗传疾病和过度增殖性疾病。
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公开(公告)号：US09315546B2
公开(公告)日：2016-04-19
申请号：US13704052
申请日：2011-06-16
IPC分类号： A61K38/08 , A61K38/10 , A61K38/16 , A61K38/22 , C07K14/575 , A61K38/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , A61K38/04 , C07K7/08 , A61K38/03 , C07K14/475 , A61K38/25 , C07K5/062 , C07K14/60 , C07K5/08 , C07K7/06 , C07K14/00 , C07K14/72
CPC分类号： C07K7/08 , A61K38/00 , A61K38/03 , A61K38/04 , A61K38/08 , A61K38/10 , A61K38/16 , A61K38/25 , C07K5/06026 , C07K5/08 , C07K7/06 , C07K14/00 , C07K14/475 , C07K14/60 , C07K14/723
摘要： The present invention provides novel peptides that can modulate the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and sub-types, isoforms and variants thereof). These peptides are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperpro-liferative disorders.
摘要翻译： 本发明提供可以调节生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的新型肽。 这些肽可用作生长素释放肽受体的拮抗剂以及反向激动剂，部分激动剂或这些活性的组合，作为用于治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病， 胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病，糖尿病，中枢神经系统疾病，遗传疾病和超高血压疾病。
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公开(公告)号：US20130172242A1
公开(公告)日：2013-07-04
申请号：US13704052
申请日：2011-06-16
CPC分类号： C07K7/08 , A61K38/00 , A61K38/03 , A61K38/04 , A61K38/08 , A61K38/10 , A61K38/16 , A61K38/25 , C07K5/06026 , C07K5/08 , C07K7/06 , C07K14/00 , C07K14/475 , C07K14/60 , C07K14/723
摘要： The present invention provides novel peptides that can modulate the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and sub-types, isoforms and variants thereof). These peptides are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.
摘要翻译： 本发明提供可以调节生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的新型肽。 这些肽可用作生长素释放肽受体的拮抗剂以及反向激动剂，部分激动剂或这些活性的组合，作为用于治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病， 胃肠道疾病，心血管疾病，肥胖和肥胖相关疾病，糖尿病，中枢神经系统疾病，遗传疾病和过度增殖性疾病。
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5.发明申请METHODS OF INHIBITING THE GHRELIN/GROWTH HORMONE SECRETATOGUE RECEPTOR PATHWAY AND USES THEREOF 有权抑制GHRELIN /生长激素分泌受体途径的方法及其用途公开(公告)号：US20120135918A1
公开(公告)日：2012-05-31
申请号：US13320408
申请日：2010-05-12
IPC分类号： A61K38/08 , A61K31/454 , A61P3/10 , C07K7/06 , C07K7/08 , A61P3/04 , A61K31/4965
CPC分类号： A61K38/08 , A61K31/00 , A61K31/404 , A61K38/10 , A61K38/16 , A61K38/25 , A61K45/06 , A61K2300/00
摘要： The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15-A16-A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a di-aminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.
摘要翻译： 本发明通过向受试者施用生长素释放肽O-酰基转移酶（GOAT）抑制剂和/或生长素释放肽受体拮抗剂来提供治疗，预防或控制受试者中肥胖症，肥胖相关病症，糖尿病和代谢综合征的方法。 本发明还提供式（VII）的生长素释放肽受体拮抗剂：A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18，其中A11，A12和A13各自独立地不存在， 氨基酸或氨基保护基; A15-A16-A17和A18各自独立地不存在或氨基酸; 并且A14是与-C（O）C1-C20烷基或与-C（O）C1-C20烷基共轭的二氨基丙酸缀合的丝氨酸，条件是存在A11，A12或A13中的至少一种。
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6.发明申请GHRELIN/GROWTH HORMONE RELEASING PEPTIDE/GROWTH HORMONE SECRETATOGUE RECEPTOR ANTAGONISTS AND USES THEREOF 有权GHRELIN / GROWTH HORMONE释放肽/生长激素分泌受体拮抗剂及其用途公开(公告)号：US20090069245A1
公开(公告)日：2009-03-12
申请号：US12298826
申请日：2007-04-30
IPC分类号： A61K38/08 , C07K7/06 , C07D401/06 , A61K31/454 , C07D403/08
CPC分类号： C07C233/75 , A61K38/00 , C07K7/02 , C07K7/06 , C07K14/60
摘要： The present invention provides novel compounds that have been demonstrated to be modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, iso forms and variants thereof). These compounds are useful as antagonists of the ghrelin receptor as well as inverse agonist, partial agonist or a combination of these activities as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, diabetes, central nervous system disorders, genetic disorders, and hyperproliferative disorders.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，其形式和变体）的调节剂的新化合物。 这些化合物可用作生长素释放肽受体的拮抗剂以及反向激动剂，部分激动剂或这些活性的组合，作为治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病， 胃肠道疾病，心血管疾病，肥胖和肥胖相关疾病，糖尿病，中枢神经系统疾病，遗传疾病和过度增殖性疾病。
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